Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AS1269574 是口服有效的GPR119激动剂,在表达人 GPR119 的 HEK293 细胞中EC50为 2.5 μM。它激活 TRPA1 阳离子通道,刺激胰高血糖素样肽-1分泌。它仅在高糖条件下特异性诱导胰腺 β 细胞分泌葡萄糖依赖性胰岛素。它在 2 型糖尿病的研究中具有价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,320 | 现货 | ||
100 mg | ¥ 4,880 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 748 | 现货 |
产品描述 | AS1269574 is a potent, orally available GPR119 agonist. AS1269574(AS 1269574) has the potential for the research of type 2 diabetes. |
体外活性 | AS1269574 had an EC(50) value of 2.5μM in HEK293 cells transiently expressing human GPR119 and enhanced insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8mM) conditions.?This contrasted with the action of the sulfonylurea glibenclamide, which also induced insulin secretion under low-glucose conditions (2.8mM)[1]. |
体内活性 | In in vivo studies, a single administration of AS1269574 to normal mice reduced blood glucose levels after oral glucose loading based on the observed insulin secretion profiles.?Significantly, AS1269574 did not affect fed and fasting plasma glucose levels in normal mice.?AS1269574 represents a novel structural class of small molecule, orally administrable GPR119 agonists with GSIS and promising potential for the treatment of type 2 diabetes[1]. |
别名 | AS 1269574 |
分子量 | 308.17 |
分子式 | C13H14BrN3O |
CAS No. | 330981-72-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (811.24 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.245 mL | 16.2248 mL | 32.4496 mL | 81.1241 mL |
5 mM | 0.649 mL | 3.245 mL | 6.4899 mL | 16.2248 mL | |
10 mM | 0.3245 mL | 1.6225 mL | 3.245 mL | 8.1124 mL | |
20 mM | 0.1622 mL | 0.8112 mL | 1.6225 mL | 4.0562 mL | |
50 mM | 0.0649 mL | 0.3245 mL | 0.649 mL | 1.6225 mL | |
100 mM | 0.0324 mL | 0.1622 mL | 0.3245 mL | 0.8112 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AS1269574 330981-72-1 Endocrinology/Hormones GPCR/G Protein Membrane transporter/Ion channel GPR TRP/TRPV Channel TRP Channel G Protein-Coupled Receptor 119 secretion AS 1269574 Inhibitor type cation AS-1269574 diabetes insulin inhibit Transient receptor potential channels glucose GPR119 channels inhibitor